1. 2-Phenyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives: new potent inhibitors of fMLP-induced neutrophil chemotaxis.
- Author
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Bruno O, Brullo C, Bondavalli F, Ranise A, Schenone S, Falzarano MS, Varani K, and Spisani S
- Subjects
- Anti-Inflammatory Agents pharmacology, Binding, Competitive, Dose-Response Relationship, Drug, Drug Design, Humans, Inhibitory Concentration 50, Kinetics, Models, Chemical, Neutrophils metabolism, Protein Binding, Signal Transduction, Chemistry, Pharmaceutical methods, Chemotaxis drug effects, N-Formylmethionine Leucyl-Phenylalanine antagonists & inhibitors, N-Formylmethionine Leucyl-Phenylalanine chemistry, Neutrophils drug effects, Pyrazoles chemistry
- Abstract
It is well known that both acute and chronic autoimmune inflammatory disorders arise following a breakdown in control of neutrophil activation and recruitment. In the search for new anti-inflammatory agents, we synthesized some new 2-phenyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives and tested them in vitro in order to evaluate their ability to interfere with human neutrophil functions. All tested compounds showed strong inhibition of fMLP-OMe-induced chemotaxis, although they appeared unable to block degranulation and the fMLP-OMe-induced respiratory burst, and were inactive in binding experiments.
- Published
- 2007
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